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br Protein acetylation Several reports show that MTX is
2021-08-31

Protein acetylation Several reports show that MTX is able to induce acetylation of histones and other proteins. Extensive studies have established that histone acetylation is primarily associated with gene activation. Acetylation occurs at lysine residues on the amino-terminal tail of the protein
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The only reported synthesis of the aminobicyclic
2021-08-31

The only reported synthesis of the aminobicyclic core of is based on bis-alkylation of a 4-amino-5,6-dihydroxypyrmidine with dibromoethane. The likelihood of poor regiocontrol/reactivity in utilizing such a transformation for the synthesis of compounds with a substituent on the dioxinyl ring led us
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We aim to apply the same technology to
2021-08-31

We aim to apply the same technology to target other collagen-binding proteins using motifs from collagens that are specific for other receptors or matrix components. Previously, we synthesized THP libraries, called Toolkits, composed of an active guest sequence flanked by five GPP host triplets that
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The discoidin domain receptors DDR and DDR
2021-08-31

The discoidin domain receptors, DDR1 and DDR2, are receptor tyrosine kinases (RTKs) that are stimulated by collagen in the extracellular matrix (ECM). Unlike most other RTKs, they form ligand-independent stable dimers that are non-covalently linked. This ECM activation induces receptor phosphorylati
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The three dimensional crystal structure of Ca
2021-08-31

The three-dimensional crystal structure of Ca2+ loaded CaM reveals a dumbbell-shaped molecule with two roughly globular lobes, the N- and C-terminal lobes linked by a long solvent-exposed helix, which has been shown by NMR to be non-helical in its central part and flexible in solution [13]. Each glo
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Although several examples of selective reduction of diazoest
2021-08-31

Although several examples of selective ap4 of α-diazoesters to α-hydrazonoesters have been described in the literature, reports on practical and general examples of such a process are scarce. In this context, there was a need to devise a mild and general method for the selective reduction of α-diaz
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Confidence with which data of animal safety toxicity studies
2021-08-31

Confidence with which data of animal safety/toxicity studies can be translated to human depends upon the knowledge that whether humans would be exposed to similar chemical entities (parent and its metabolites) as the animals exposed during toxicity studies. In this regard, in vitro qualitative evalu
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run out of As the principal receptors for
2021-08-31

As the principal receptors for regulating the inflammatory process in mammals, CXCR1 and CXCR2 have an important role in regulating the trafficking of phagocytes such as neutrophils, monocytes and macrophages (Viola and Luster, 2008). The evidence gathered to date from fish studies are in agreement
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The physiological role of the UCNs in the regulation
2021-08-31

The physiological role of the UCNs in the regulation of the HPA axis is still under debate (Fekete and Zorrilla, 2007, Suda et al., 2004). UCN 1 was proved to increase the plasma ACTH and corticosterone levels in rats (Bagosi et al., 2014, Vaughan et al., 1995), whereas UCN 2 and UCN 3 were shown to
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Cefpodoxime Proxetil To simulate the inhibition of the enzym
2021-08-31

To simulate the inhibition of the enzyme by organophosphorus, carbamate insecticides or nerve agents, a reversible cholinesterase inhibitor physostigmine was used for most experiments for safety reasons. However, the results of the measurements were verified using the soman organophosphate, which is
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With regards to what might represent
2021-08-31

With regards to what might represent a typical “baseline” ChE (or AChE) activity in Saccostrea sp., it mibefradil should be remembered that the observed enzyme responses were obtained in laboratory exposures, over a narrow experimental window (96h), with specimens collected over the course of a wee
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Together the data suggests that
2021-08-31

Together, the data suggests that more work needs to be done to establish the role of PARP inhibitors in Ewing sarcoma. As a single agent, there is some activity in Ewing sarcoma cell lines and a highly statistically significant relationship between olaparib sensitivity and EWS–FLI1 expression. Howev
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br PFL AE as a
2021-08-31

PFL-AE as a model for the GRE–AEs Most of the GRE–AEs have proven difficult to study due to instability, difficulty in overexpression, lability of the iron-sulfur cluster, or other reasons. PFL-AE is the exception, and after the initial discovery of the iron–sulfur cluster in this enzyme [60], co
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br Introduction Protein modification by ubiquitin and ubiqui
2021-08-30

Introduction Protein modification by ubiquitin and ubiquitin-like proteins is one of the most common and important regulatory mechanisms in biology (Finley et al., 2004, Pickart, 2004). Ubiquitination is carried out by an enzymatic cascade consisting of three steps. In the first step, ubiquitin i
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br Results br Discussion MSCs derived from
2021-08-30

Results Discussion MSCs derived from the bone marrow and adipose tissue have been shown to promote the growth and metastatic ability of breast cancer and other human malignancies, but the mechanisms are incompletely understood (Barcellos-Hoff et al., 2013, Cuiffo et al., 2014, Del Pozo Martin
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